Pharmacokinetics and pharmacodynamics of exenatide extended-release after single and multiple dosing.

Fineman M, Flanagan S, Taylor K, Aisporna M, Shen LZ, Mace KF, Walsh B, Diamant M, Cirincione B, Kothare P, Li WI, MacConell L

Clinical pharmacokinetics1 Jan 2011Cited by 116 (Europe PMC)

PMID21142268DOI10.2165/11585880-000000000-00000PepBankPUB-21142268

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Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study12

11 results from studies that gave the peptide. 11 results from people.

01HumanNon-randomized trialPharmacokinetics
In patients with type 2 diabetes, exenatide ER exposure increased with single-dose size.
In plain wordsIn patients with type 2 diabetes, larger single exenatide ER doses produced greater drug exposure than lower doses.
Peptide
Exenatide (exendin-4)
Outcome
IncreaseDose-related exposure
Study
n: not reported in source
Comparator
lower single doses
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
2.5, 5, 7 or 10 mg · subcutaneous · single dose; observed 12 weeksAs given in this study (human).
Source sentences
Summary
Exenatide exposure increased with dose (2.5 mg, 5 mg, 7 mg or 10 mg) and exhibited a multiple-peak profile over approximately 10 weeks.
2 context sentences(design, population, supporting numbers)
Summary · context
The pharmacokinetic and safety effects of single-dose subcutaneous administration of exenatide ER (2.5 mg, 5 mg, 7 mg or 10 mg) versus placebo were studied over a period of 12 weeks in patients with type 2 diabetes.
Summary · context
Patients with type 2 diabetes participated in either a single-dose trial (n = 62) or a repeated-administration trial (n = 45).
Report a problemFND-2114226801
02HumanNon-randomized trialPharmacokinetics
In patients with type 2 diabetes, single-dose exenatide ER exhibited a multiple-peak exposure profile over approximately 10 weeks.
In plain wordsIn patients with type 2 diabetes, single-dose exenatide ER exposure had several peaks over approximately 10 weeks.
Peptide
Exenatide (exendin-4)
Outcome
Not applicableMultiple-peak exposure profile
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
2.5, 5, 7 or 10 mg · subcutaneous · single dose; observed 12 weeksAs given in this study (human).
Source sentences
Summary
Exenatide exposure increased with dose (2.5 mg, 5 mg, 7 mg or 10 mg) and exhibited a multiple-peak profile over approximately 10 weeks.
2 context sentences(design, population, supporting numbers)
Summary · context
The pharmacokinetic and safety effects of single-dose subcutaneous administration of exenatide ER (2.5 mg, 5 mg, 7 mg or 10 mg) versus placebo were studied over a period of 12 weeks in patients with type 2 diabetes.
Summary · context
Patients with type 2 diabetes participated in either a single-dose trial (n = 62) or a repeated-administration trial (n = 45).
Report a problemFND-2114226802
03HumanNon-randomized trialPharmacokinetics
In patients with type 2 diabetes, weekly exenatide ER pharmacokinetics confirmed predictions from single-dose data.
In plain wordsIn patients with type 2 diabetes, weekly exenatide ER drug levels agreed with predictions from single-dose data.
Peptide
Exenatide (exendin-4)
Outcome
Not applicableAgreement with predicted multiple-dose pharmacokinetics
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.8 mg or 2 mg weekly · subcutaneous · 15 weeksAs given in this study (human).
Source sentences
Summary
Multiple-dosing pharmacokinetics were predicted from superpositioning of single-dose data; weekly administration of exenatide ER 0.8 mg and 2 mg for 15 weeks confirmed the predictions.
2 context sentences(design, population, supporting numbers)
Summary · context
A second clinical study investigated the pharmacokinetics, pharmacodynamics and safety of weekly exenatide ER subcutaneous injections (0.8 mg or 2 mg) versus placebo in patients with type 2 diabetes over a period of 15 weeks.
Summary · context
Patients with type 2 diabetes participated in either a single-dose trial (n = 62) or a repeated-administration trial (n = 45).
Report a problemFND-2114226803
04HumanNon-randomized trialPharmacokinetics
In patients with type 2 diabetes, weekly exenatide ER reached steady-state plasma concentrations after 6-7 weeks.
In plain wordsIn patients with type 2 diabetes, weekly exenatide ER reached stable plasma levels after 6-7 weeks.
Peptide
Exenatide (exendin-4)
Outcome
Not applicableTime to steady-state concentration
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
0.8 mg or 2 mg weekly · subcutaneous · 15 weeksAs given in this study (human).
Measurements
Time to steady state
6 to 7 weeks
weekly dosing
Source sentences
Summary
Weekly dosing resulted in steady-state plasma exenatide concentrations after 6-7 weeks.
2 context sentences(design, population, supporting numbers)
Summary · context
A second clinical study investigated the pharmacokinetics, pharmacodynamics and safety of weekly exenatide ER subcutaneous injections (0.8 mg or 2 mg) versus placebo in patients with type 2 diabetes over a period of 15 weeks.
Summary · context
Patients with type 2 diabetes participated in either a single-dose trial (n = 62) or a repeated-administration trial (n = 45).
Report a problemFND-2114226804
05HumanNon-randomized trialEfficacy outcome
In patients with type 2 diabetes, exenatide ER 0.8 mg reduced fasting glucose versus placebo.
In plain wordsIn patients with type 2 diabetes, exenatide ER 0.8 mg reduced fasting blood sugar compared with placebo.
Peptide
Exenatide (exendin-4)
Outcome
DecreaseFasting plasma glucose with 0.8 mg
Study
n: not reported in source
Comparator
placebo
Outcome group
Glycemic control · Metabolic and weight
Studied dose
0.8 mg weekly · subcutaneous · 15 weeksAs given in this study (human).
Measurements
Fasting glucose change
−42.7 mg/dL
0.8 mg
Reported variability
15.7 mg/dL
0.8 mg
Source sentences
Summary
Fasting plasma glucose levels were reduced similarly with both doses after 15 weeks (-42.7 ± 15.7 mg/dL with the 0.8 mg dose and -39.0 ± 9.3 mg/dL with the 2 mg dose; both p < 0.001 vs placebo),
2 context sentences(design, population, supporting numbers)
Summary · context
A second clinical study investigated the pharmacokinetics, pharmacodynamics and safety of weekly exenatide ER subcutaneous injections (0.8 mg or 2 mg) versus placebo in patients with type 2 diabetes over a period of 15 weeks.
Summary · context
Patients with type 2 diabetes participated in either a single-dose trial (n = 62) or a repeated-administration trial (n = 45).
Report a problemFND-2114226805
06HumanNon-randomized trialEfficacy outcome
In patients with type 2 diabetes, exenatide ER 2 mg reduced fasting glucose versus placebo.
In plain wordsIn patients with type 2 diabetes, exenatide ER 2 mg reduced fasting blood sugar compared with placebo.
Peptide
Exenatide (exendin-4)
Outcome
DecreaseFasting plasma glucose with 2 mg
Study
n: not reported in source
Comparator
placebo
Outcome group
Glycemic control · Metabolic and weight
Studied dose
2 mg weekly · subcutaneous · 15 weeksAs given in this study (human).
Measurements
Fasting glucose change
−39 mg/dL
2 mg
Reported variability
9.3 mg/dL
2 mg
Source sentences
Summary
Fasting plasma glucose levels were reduced similarly with both doses after 15 weeks (-42.7 ± 15.7 mg/dL with the 0.8 mg dose and -39.0 ± 9.3 mg/dL with the 2 mg dose; both p < 0.001 vs placebo),
2 context sentences(design, population, supporting numbers)
Summary · context
A second clinical study investigated the pharmacokinetics, pharmacodynamics and safety of weekly exenatide ER subcutaneous injections (0.8 mg or 2 mg) versus placebo in patients with type 2 diabetes over a period of 15 weeks.
Summary · context
Patients with type 2 diabetes participated in either a single-dose trial (n = 62) or a repeated-administration trial (n = 45).
Report a problemFND-2114226806
07HumanNon-randomized trialEfficacy outcome
In patients with type 2 diabetes, exenatide ER 2 mg reduced weight versus placebo.
In plain wordsIn patients with type 2 diabetes, exenatide ER 2 mg reduced weight compared with placebo.
Peptide
Exenatide (exendin-4)
Outcome
DecreaseBodyweight with 2 mg
Study
n: not reported in source
Comparator
placebo
Outcome group
Body weight · Metabolic and weight
Studied dose
2 mg weekly · subcutaneous · 15 weeksAs given in this study (human).
Measurements
Bodyweight change
−3.8 kg
2 mg
Reported variability
1.4 kg
2 mg
Source sentences
Summary
The 2 mg dose reduced bodyweight (-3.8 ± 1.4 kg; p < 0.05 vs placebo) and postprandial glucose excursions.
2 context sentences(design, population, supporting numbers)
Summary · context
A second clinical study investigated the pharmacokinetics, pharmacodynamics and safety of weekly exenatide ER subcutaneous injections (0.8 mg or 2 mg) versus placebo in patients with type 2 diabetes over a period of 15 weeks.
Summary · context
Patients with type 2 diabetes participated in either a single-dose trial (n = 62) or a repeated-administration trial (n = 45).
Report a problemFND-2114226808
08HumanNon-randomized trialEfficacy outcome
In patients with type 2 diabetes, exenatide ER 2 mg reduced postprandial glucose excursions.
In plain wordsIn patients with type 2 diabetes, exenatide ER 2 mg reduced blood sugar rises after meals.
Peptide
Exenatide (exendin-4)
Outcome
DecreasePostprandial glucose excursions with 2 mg
Study
n: not reported in source
Outcome group
Glycemic control · Metabolic and weight
Studied dose
2 mg weekly · subcutaneous · 15 weeksAs given in this study (human).
Source sentences
Summary
The 2 mg dose reduced bodyweight (-3.8 ± 1.4 kg; p < 0.05 vs placebo) and postprandial glucose excursions.
2 context sentences(design, population, supporting numbers)
Summary · context
A second clinical study investigated the pharmacokinetics, pharmacodynamics and safety of weekly exenatide ER subcutaneous injections (0.8 mg or 2 mg) versus placebo in patients with type 2 diabetes over a period of 15 weeks.
Summary · context
Patients with type 2 diabetes participated in either a single-dose trial (n = 62) or a repeated-administration trial (n = 45).
Report a problemFND-2114226809
09HumanNon-randomized trialEfficacy outcome
In patients with type 2 diabetes, exenatide ER 0.8 mg reduced HbA1c versus placebo.
In plain wordsIn patients with type 2 diabetes, exenatide ER 0.8 mg reduced long-term blood sugar compared with placebo.
Peptide
Exenatide (exendin-4)
Outcome
DecreaseHbA1c with 0.8 mg
Study
n: not reported in source
Comparator
placebo
Outcome group
Glycemic control · Metabolic and weight
Studied dose
0.8 mg weekly · subcutaneous · 15 weeksAs given in this study (human).
Measurements
HbA1c change
−1.4%
0.8 mg
Reported variability
0.3%
0.8 mg
Baseline HbA1c
8.6%
0.8 mg
Source sentences
Summary
Glycosylated haemoglobin (HbA(1c)) levels were reduced with the 0.8 mg dose (-1.4 ± 0.3%; baseline 8.6%) and with the 2 mg dose (-1.7 ± 0.3%; baseline 8.3%) [both p < 0.001 vs placebo].
2 context sentences(design, population, supporting numbers)
Summary · context
A second clinical study investigated the pharmacokinetics, pharmacodynamics and safety of weekly exenatide ER subcutaneous injections (0.8 mg or 2 mg) versus placebo in patients with type 2 diabetes over a period of 15 weeks.
Summary · context
Patients with type 2 diabetes participated in either a single-dose trial (n = 62) or a repeated-administration trial (n = 45).
Report a problemFND-2114226810
10HumanNon-randomized trialEfficacy outcome
In patients with type 2 diabetes, exenatide ER 2 mg reduced HbA1c versus placebo.
In plain wordsIn patients with type 2 diabetes, exenatide ER 2 mg reduced long-term blood sugar compared with placebo.
Peptide
Exenatide (exendin-4)
Outcome
DecreaseHbA1c with 2 mg
Study
n: not reported in source
Comparator
placebo
Outcome group
Glycemic control · Metabolic and weight
Studied dose
2 mg weekly · subcutaneous · 15 weeksAs given in this study (human).
Measurements
HbA1c change
−1.7%
2 mg
Reported variability
0.3%
2 mg
Baseline HbA1c
8.3%
2 mg
Source sentences
Summary
Glycosylated haemoglobin (HbA(1c)) levels were reduced with the 0.8 mg dose (-1.4 ± 0.3%; baseline 8.6%) and with the 2 mg dose (-1.7 ± 0.3%; baseline 8.3%) [both p < 0.001 vs placebo].
2 context sentences(design, population, supporting numbers)
Summary · context
A second clinical study investigated the pharmacokinetics, pharmacodynamics and safety of weekly exenatide ER subcutaneous injections (0.8 mg or 2 mg) versus placebo in patients with type 2 diabetes over a period of 15 weeks.
Summary · context
Patients with type 2 diabetes participated in either a single-dose trial (n = 62) or a repeated-administration trial (n = 45).
Report a problemFND-2114226811
11HumanNon-randomized trialSafety outcome
In patients with type 2 diabetes receiving exenatide ER, adverse events were generally transient and mild to moderate.
In plain wordsIn patients with type 2 diabetes receiving exenatide ER, adverse events were generally temporary and mild to moderate.
Peptide
Exenatide (exendin-4)
Outcome
Not applicableAdverse event severity and duration
Study
n: not reported in source
Outcome group
Adverse events · Whole body
Studied dose
Dose not stated · subcutaneousAs given in this study (human).
Source sentences
Summary
Adverse events were generally transient and mild to moderate in intensity.
1 context sentence(design, population, supporting numbers)
Summary · context
Patients with type 2 diabetes participated in either a single-dose trial (n = 62) or a repeated-administration trial (n = 45).
Report a problemFND-2114226812

Studies that did not test the peptide alone1

In this study, Exenatide (exendin-4) was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking Exenatide (exendin-4).

12HumanNot a test of Exenatide (exendin-4) aloneNon-randomized trialPharmacokinetics
In exposure-response modeling, the exenatide ER concentration producing half-maximal fasting glucose effects was 56.8 pg/mL.
In plain wordsIn computer modeling, exenatide ER produced half of its maximum fasting blood sugar effect at 56.8 pg/mL.
Peptide
Exenatide (exendin-4)
Outcome
Not applicableFasting glucose exposure-response EC50
Study
n: not reported in source
integrated exposure-response analysis of clinical exenatide ER data
Outcome group
Pharmacokinetics · Pharmacology
Measurements
EC50
56.8 pg/mL
fasting plasma glucose
Source sentences
Summary
and the integrated exposure-response analysis demonstrated that the drug concentration producing 50% of the maximum effect (EC(50)) on fasting plasma glucose was 56.8 pg/mL
1 context sentence(design, population, supporting numbers)
Summary · context
Patients with type 2 diabetes participated in either a single-dose trial (n = 62) or a repeated-administration trial (n = 45).
In this study, Exenatide (exendin-4) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Exenatide (exendin-4).
Report a problemFND-2114226807

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Registered trials1

Trials this study reports on, or that list this study as a reference. Registry data from ClinicalTrials.gov.

1 trial · 1 completed · source ClinicalTrials.gov (opens in a new tab)

CompletedPhase 2NCT00103935

Study Examining Exenatide Long-Acting Release in Subjects With Type 2 Diabetes

AstraZenecan = 45Feb 2005 to Oct 2005

Type 2 Diabetes Mellitus

Trial page ClinicalTrials.govUpdated 24 Feb 2015

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
22 Oct 2026, 02:26 UTC
Study results updated
Version 1
21 Oct 2026, 18:59 UTC
First added · source update from Europe PMC

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